|1-(4'-(3-甲基-4-(((((R)-1-苯基乙基)氧基)羰基)氨基)异恶唑-5-基)联苯-4-基)环丙烷羧酸|CsnPharm

CAS No.: 1257213-50-5

BMS-986020 Catalog No. CSN18842

Synonyms: AM152;AM-000152;AP-3152 free acid

BMS-986020 is an LPA1 antagonist.

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技术信息

生物活性

描述Idiopathic pulmonary fibrosis (IPF) causes irreversible loss of lung function. The lysophosphatidic acid receptor 1 (LPA₁) pathway is implicated in IPF etiology. BMS-986020 is a high-affinity LPA₁ antagonist under assessment in a phase 2 study in patients with IPF^[2]. A BMS-986020 concentration-dependent displacement of [¹⁸F]BMT-083133 binding was observed in LPA1⁺ cells and lung sections. At 0.1 nM of BMS-986020, the percent displacement in healthy mice, bleomycin mice, and IPF lungs was 18%, 24%, and 31%, respectively; and at 10 nM, the percent displacement was 73%, 76%, and 64%, respectively^[3]. Patients treated with BMS-986020 (600 mg for 26 weeks) experienced a significantly slower rate of decline in FVC vs placebo. Dose-related elevations in hepatic enzymes were observed in both BMS-986020 treatment groups^[2].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01766817	Idiopathic Pulmonary Fibrosis	Phase 2	Completed	-	-
NCT02101125	Immunosuppression For Disease	Phase 1	Completed	-	United States, Texas ... more >> Healthcare Discoveries, Llc D/B/A Icon Development Solutions San Antonio, Texas, United States, 78209 Collapse <<
NCT02068053	Immunosuppression For Disease	Phase 1	Completed	-	-

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参考文献

[1] Kihara Y, Mizuno H, et al. Lysophospholipid receptors in drug discovery. Exp Cell Res. 2015 May 1;333(2):171-7.
[2] Palmer SM, Snyder L, Todd JL, et al. Randomized, Double-Blind, Placebo-Controlled, Phase 2 Trial of BMS-986020, a Lysophosphatidic Acid Receptor Antagonist for the Treatment of Idiopathic Pulmonary Fibrosis. Chest. 2018;154(5):1061‐1069
[3] Autoradiographic evaluation of [¹⁸F]BMT-083133, a lysophosphatidic acid receptor 1 (LPA1) radioligand

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0724 mL
- 10.3621 mL
- 20.7242 mL
- 5 mM
- 0.4145 mL
- 2.0724 mL
- 4.1448 mL
- 10 mM
- 0.2072 mL
- 1.0362 mL
- 2.0724 mL

技术信息

CAS号

1257213-50-5

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H26N2O5

运输

蓝冰

分子量

482.53

别名

AM152;AM-000152;AP-3152 free acid

溶解度

DMSO	55.0 mg/mL (114.0 mM)
Water	insoluble

动物实验配方

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